This Phase I study is designed to evaluate the safety, tolerability, and pharmacokinetic profile of BT01001 Ophthalmic Solution in healthy adult volunteers. The primary objectives are to assess the safety and tolerability of single and multiple ascending doses and to characterize the pharmacokinetics of BT01001 Ophthalmic Solution following topical ocular administration. This is a randomized, double-blind, placebo-controlled, dose-escalation trial consisting of four ascending dose cohorts. Each cohort will enroll eight participants, including six receiving BT01001 Ophthalmic Solution and 2 receiving Placebo.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
QUADRUPLE
Enrollment
32
BT01001 Ophthalmic Solution will be administered as topical instillation into the right eye of each subject according to the assigned dosing schedule.
BT01001 Ophthalmic Solution will be administered as topical instillation into the right eye of each subject according to the assigned dosing schedule.
BT01001 Ophthalmic Solution will be administered as topical instillation into the right eye of each subject according to the assigned dosing schedule.
Placebo BT01001 Ophthalmic Solution will be administered as a topical instillation into the right eye of each subject following the same dosing schedule as the active treatment.
Shanghai General Hospital
Shanghai, China
RECRUITINGNumber of Participants With Adverse Events as Assessed by CTCAE V5.0
Any AE event related to study treatment
Time frame: after dosing up to 14 days/12 days
Dose-Limiting Toxicity
≥CTCAE 2 ocular adverse events or· \>CTCAE 3 non-ocular· adverse events· assessed with·CTCAE·5.0
Time frame: SAD: after dosing up to 2 days; MAD: after dosing up to 8 days
Measured Area Under the Curve (AUC)
SAD(dose 1-3): at Day 1 pre-dose, 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 12h, 24h. MAD(dose 1-3): at Day 8 pre-dose(before the first dose), Day 8 pre-dose(before the second dose), Day 9 pre-dose(before the first drop), 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 12h, 24h. MAD(dose 4): at Day 6 pre-dose(before the second dose), Day 6 pre-dose(before the third dose), Day 7 pre-dose(before the first dose), 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 12h, 24h.
Time frame: SAD(dose 1-3): Day 1, Day 2; MAD(dose 1-3): Day 8, Day 9, Day 10; MAD(dose 4): Day 6, Day 7,Day 8;
Time to Maximum Plasma Concentration (Tmax)
SAD(dose 1-3): at Day 1 pre-dose, 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 12h, 24h. MAD(dose 1-3): at Day 8 pre-dose(before the first dose), Day 8 pre-dose(before the second dose), Day 9 pre-dose(before the first drop), 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 12h, 24h. MAD(dose 4): at Day 6 pre-dose(before the second dose), Day 6 pre-dose(before the third dose), Day 7 pre-dose(before the first dose), 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 12h, 24h.
Time frame: SAD(dose 1-3): Day 1, Day 2; MAD(dose 1-3): Day 8, Day 9, Day 10; MAD(dose 4): Day 6, Day 7,Day 8;
Maximum Plasma Concentration (Cmax)
SAD(dose 1-3): at Day 1 pre-dose, 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 12h, 24h. MAD(dose 1-3): at Day 8 pre-dose(before the first dose), Day 8 pre-dose(before the second dose), Day 9 pre-dose(before the first drop), 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 12h, 24h. MAD(dose 4): at Day 6 pre-dose(before the second dose), Day 6 pre-dose(before the third dose), Day 7 pre-dose(before the first dose), 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 12h, 24h.
Time frame: SAD(dose 1-3): Day 1, Day 2; MAD(dose 1-3): Day 8, Day 9, Day 10; MAD(dose 4): Day 6, Day 7,Day 8;
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